KENDALL NETTLES PRT TIME

肯德尔·荨麻 PRT 时间

• 批准号: 7954388
• 负责人: Kendall W Nettles
• 金额: $ 0.02万
• 依托单位: STANFORD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2009
• 资助国家: 美国
• 起止时间: 2009-03-01 至 2010-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7954388
• 关键词: Agonist; Binding; Computer Retrieval of Information on Scientific Projects Database; Crystallography; Diabetes Mellitus; Drug Design; Estrogen Receptor alpha; Funding; Goals; Grant; Hormones; Institution; Ligand Binding Domain; Ligands; Liver diseases; Malignant Neoplasms; Nuclear; Nuclear Hormone Receptors; Obesity; PPAR gamma; Peroxisome Proliferator-Activated Receptors; Protein Family; Proteins; Research; Research Personnel; Resources; Source; Structure; Time; United States National Institutes of Health; Work; base; human disease; receptor; structural biology; synchrotron radiation; transcription factor

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. The research focuses on the nuclear hormone family of proteins. Nuclear hormone receptor proteins are ligand inducible transcription factors. Nuclear hormone receptors are involved in several human diseases including cancer, liver disease, obesity, and diabetes. Specifically, we are working with the ligand binding domains of estrogen receptor alpha (ERalpha LBD) and peroxisome proliferator activated receptor gamma (PPAR-gamma). Our goal is to acquire a better understanding of the partial agonism mechanism of these proteins in order to carry out structure based drug design. Experimentally, we desire to characterize several partial agonists bound to PPAR and ER, solve the structures by x-ray crystallography, dissect the atomic level interactions of the ligands, and compare and contrast these interactions and induced allostery with full agonists and antagonists.

该副本是利用众多研究子项目之一 由NIH/NCRR资助的中心赠款提供的资源。子弹和 调查员（PI）可能已经从其他NIH来源获得了主要资金， 因此可以在其他清晰的条目中代表。列出的机构是 对于中心，这不一定是调查员的机构。 该研究的重点是蛋白质的核激素家族。 核激素受体蛋白是配体诱导转录因子。 核激素受体参与了几种人类疾病，包括癌症，肝病，肥胖和糖尿病。 具体而言，我们正在使用雌激素受体α（Eralpha LBD）和过氧化物酶体增殖物激活受体伽马（PPAR-GAMMA）的配体结合结构域（PPAR-GAMMA）。 我们的目标是更好地了解这些蛋白质的部分激动剂机制，以进行基于结构的药物设计。 在实验上，我们希望表征与PPAR和ER结合的几种部分激动剂，通过X射线晶体学解决结构，剖析配体的原子水平相互作用，并比较和对比这些相互作用，并与完全的激动剂和拮抗剂进行变构。